Design and Synthesis of Fused Pyridine Building Blocks for Automated Library Generation

Abstract

We demonstrate that a diboration‐electrocyclization sequence provides access to a range of pyridine‐fused, small‐molecule boronic ester building blocks, and that these are amenable to high‐throughput synthesis leading to biaryl and ether‐linked compound libraries. Moreover, the implementation of an integrated physicochemical and ADME profiling workflow allows accelerated design of novel lead compounds for application in drug‐discovery projects.